Synthesis, characterization and biological evaluation of novel dihydropyranoindoles improving the anticancer effects of HDAC inhibitors

Basit Öğe Kaydı
dc.authorid0000-0002-3909-0694en_US
dc.contributor.authorBingül, Murat
dc.contributor.authorArndt, Greg M.
dc.contributor.authorMarshall, Glenn M.
dc.contributor.authorCheung, Belamy
dc.contributor.authorKumar, Naresh Sampath
dc.contributor.authorBlack, David St Clair
dc.date.accessioned2021-09-02T11:52:44Z
dc.date.available2021-09-02T11:52:44Z
dc.date.issued2020en_US
dc.departmentDicle Üniversitesi, Eczacılık Fakültesi, Temel Eczacılık Bilimleri Bölümüen_US
dc.descriptionWOS:000530248700120
dc.descriptionPMID: 32197360
dc.description.abstractThe dihydropyranoindole scaffold was identified as a promising target for improving the anti-cancer activity of HDAC inhibitors from the preliminary screening of a library of compounds. A suitable methodology has been developed for the preparation of novel dihydropyranoindoles via the Hemetsberger indole synthesis using azido-phenylacrylates, derived from the reaction of corresponding alkynyl-benzaldehydes with methyl azidoacetate, followed by thermal cyclization in high boiling solvents. Anti-cancer activity of all the newly synthesized compounds was evaluated against the SH-SY5Y and Kelly neuroblastoma cells as well as the MDA-MB-231 and MCF-7 breast adenocarcinoma cell lines. Biological studies showed that the tetracyclic systems had significant cytotoxic activity at higher concentration against the neuroblastoma cancer cells. More importantly, these systems, at the lower concentration, considerably enhanced the SAHA toxicity. In addition to that, the toxicity of designated systems on the healthy human cells was found to be significantly less than the cancer cells. © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).en_US
dc.identifier.citationBingül, M., Arndt, G. M., Marshall, G. M., Cheung, B. ve Kumar, N. S. (2020). Synthesis, characterization and biological evaluation of novel dihydropyranoindoles improving the anticancer effects of HDAC inhibitors. Molecules, 25(6), 1377.en_US
dc.identifier.doi10.3390/molecules25061377
dc.identifier.issn1420-3049
dc.identifier.issue6en_US
dc.identifier.pmid32197360
dc.identifier.scopus2-s2.0-85082062815
dc.identifier.scopusqualityQ1
dc.identifier.startpage1377en_US
dc.identifier.urihttps://www.mdpi.com/1420-3049/25/6/1377
dc.identifier.urihttps://hdl.handle.net/11468/7417
dc.identifier.volume25en_US
dc.identifier.wosWOS:000530248700120
dc.identifier.wosqualityQ2
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.institutionauthorBingül, Murat
dc.language.isoenen_US
dc.publisherMDPI AGen_US
dc.relation.ispartofMolecules
dc.relation.publicationcategoryKonferans Öğesi - Uluslararası - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectBreast canceren_US
dc.subjectDihydropyranoindoleen_US
dc.subjectHDAC inhibitorsen_US
dc.subjectNeuroblastomaen_US
dc.titleSynthesis, characterization and biological evaluation of novel dihydropyranoindoles improving the anticancer effects of HDAC inhibitorsen_US
dc.titleSynthesis, characterization and biological evaluation of novel dihydropyranoindoles improving the anticancer effects of HDAC inhibitors
dc.typeArticleen_US

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